Mechanism of inhibition of P-glycoprotein mediated efflux by Pluronic P123/F127 block copolymers: Relationship between copolymer concentration and inhibitory activity

2013 ◽  
Vol 83 (2) ◽  
pp. 266-274 ◽  
Author(s):  
Zhang Wei ◽  
Shi Yuan ◽  
Junguo Hao ◽  
Xiaoling Fang
Keyword(s):  
Block Copolymers ◽  
Inhibitory Activity ◽  
Copolymer Concentration ◽  
Pluronic P123 ◽  
P Glycoprotein ◽  
Mechanism Of Inhibition

Mechanism of inhibition of succinate oxidase by products of oxidation of o-dihydroxycoumarins

1980 ◽  
Vol 45 (2) ◽  
pp. 641-652
Author(s):  
Petr Zbořil
Keyword(s):  
Inhibitory Activity ◽  
Oxidase Activity ◽  
Enzyme Preparation ◽  
Inhibitory Effects ◽  
Anaerobic Conditions ◽  
Long Period ◽  
Mechanism Of Inhibition ◽  
Intermediary Product ◽  
Succinate Oxidase ◽  
By Products

Semiquinone is an intermediary product of the oxidation of daphnetin (7,8-dihydroxycoumarin) and esculetin (6,7-dihydroxycoumarin) by diphenol oxidase; its concentration rapidly decreases. When the oxidation is effected by ferricytochrome c, the concentration of the semiquinone remains practically constant for a long period. Similarly, the ability of the products of daphnetin oxidation by diphenol oxidase to inhibit succinate oxidase activity in mitochondrial fragments rapidly decreases with time; the decrease is considerably slower in the case of cytochrome c. The inhibitory activity of the product decreases with time also during esculetin oxidation by ferricyanide. This indicates that the inhibitory effects must be ascribed predominantly to the semiquinone, the quinone is less efficient. The inhibition of succinate oxidase or succinate dehydrogenase was strongly decreased when the enzyme preparation of Keilin and Hartree was incubated with esculetin and ferricyanide in the presence of KCN or under anaerobic conditions. This demonstrates that the reaction of the inhibitor with the enzyme either involves subsequent oxidations or that the inhibitor preferentially reacts with the oxidized form of the sensitive component of the respiratory chain. The second alternative is very little probable since there is no correlation between the degree of inhibition and the binding of the inhibitor to mitochondrial fragments.

Coarse-grained simulation of the self-assembly of lipid vesicles concomitantly with novel block copolymers with multiple tails

Soft Matter ◽  
2021 ◽  
Author(s):  
Alexander Kantardjiev
Keyword(s):  
Molecular Dynamics ◽  
Block Copolymers ◽  
Self Assembly ◽  
Lipid Vesicles ◽  
The Self ◽  
Coarse Grained ◽  
Copolymer Concentration ◽  
Copolymer Structure ◽  
Coarse Grained Molecular Dynamics

We carried out a series of coarse-grained molecular dynamics liposome-copolymer simulations with varying extent of copolymer concentration in an attempt to understand the effect of copolymer structure and concentration on vesicle self-assembly and stability.

scholarly journals Drug-induced conversion of liver haem into modified porphyrins. Evidence for two classes of products

1980 ◽  
Vol 187 (1) ◽  
pp. 285-288 ◽  
Author(s):  
F De Matteis ◽  
A H Gibbs
Keyword(s):  
Inhibitory Activity ◽  
Spectral Properties ◽  
Drug Induced ◽  
Mechanism Of Inhibition ◽  
Green Pigments

A porphyrin with inhibitory activity towards protohaem ferro-lyase (EC 4.99.1.1) was isolated from the liver of mice given either griseofulvin or isogriseofulvin. This porphyrin resembles closely in chromatographic and spectral properties the inhibitory pigment isolated after treatment with 3,5-diethoxycarbonyl-1,4-dihydrocollidine, but differs from other green pigments that do not inhibit protohaem ferro-lyase. A hypothesis is proposed to account for the differences in properties between the two groups of pigments and for the mechanism of inhibition of the enzyme.

Small molecule-mediated self-assembly behaviors of Pluronic block copolymers in aqueous solution: impact of hydrogen bonding on the morphological transition of Pluronic micelles

Soft Matter ◽  
2020 ◽  
Vol 16 (1) ◽  
pp. 142-151 ◽  
Author(s):  
Haiyan Luo ◽  
Kun Jiang ◽  
Xiangfeng Liang ◽  
Huizhou Liu ◽  
Yingbo Li
Keyword(s):  
Aqueous Solution ◽  
Hydrogen Bonding ◽  
Block Copolymers ◽  
Small Molecules ◽  
Small Molecule ◽  
Propyl Gallate ◽  
Self Assembly ◽  
Morphological Transition ◽  
Propyl Paraben ◽  
Pluronic P123

The influence of hydrogen bonding on the morphological transition of Pluronic P123 micelles is experimentally and theoretically investigated by introducing three small molecules, i.e. propyl benzoate (PB), propyl paraben (PP) and propyl gallate (PG).

scholarly journals Quantitative Structure–Activity Relationships for the Flavonoid-Mediated Inhibition of P-Glycoprotein in KB/MDR1 Cells

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1661 ◽  
Author(s):  
Mengmeng Xia ◽  
Yajing Fang ◽  
Weiwei Cao ◽  
Fuqiang Liang ◽  
Siyi Pan ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Qsar Model ◽  
Quantitative Structure Activity Relationship ◽  
Quantitative Structure ◽  
Glycoprotein P ◽  
Chemotherapy Drugs ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Daily Diet ◽  
Low Toxicity

P-glycoprotein (P-gp) serves as a therapeutic target for the development of inhibitors to overcome multidrug resistance (MDR) in cancer cells. In order to enhance the uptake of chemotherapy drugs, larger amounts of P-gp inhibitors are required. Besides several chemically synthesized P-gp inhibitors, flavonoids as P-gp inhibitors are being investigated, with their advantages including abundance in our daily diet and a low toxicity. The cytotoxicity of daunorubicin (as a substrate of P-gp) to KB/MDR1 cells and the parental KB cells was measured in the presence or absence of flavonoids. A two-dimensional quantitative structure–activity relationship (2D-QSAR) model was built with a high cross-validation coefficient (Q2) value of 0.829. Descriptors including vsurf_DW23, E_sol, Dipole and vsurf_G were determined to be related to the inhibitory activity of flavonoids. The lack of 2,3-double bond, 3′-OH, 4′-OH and the increased number of methoxylated substitutions were shown to be beneficial for the inhibition of P-gp. These results are important for the screening of flavonoids for inhibitory activity on P-gp.

Cytocompatibility and P-glycoprotein Inhibition of Block Copolymers: Structure–Activity Relationship

2013 ◽  
Vol 10 (8) ◽  
pp. 3232-3241 ◽  
Author(s):  
A. Cambón ◽  
J. Brea ◽  
M. I. Loza ◽  
C. Alvarez-Lorenzo ◽  
A. Concheiro ◽  
...  
Keyword(s):  
Block Copolymers ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Glycoprotein Inhibition

P-Glycoprotein Inhibitory Activity of Lipophilic Constituents of Echinacea pallida Roots in a Human Proximal Tubular Cell Line

Planta Medica ◽  
2008 ◽  
Vol 74 (3) ◽  
pp. 264-266 ◽  
Author(s):  
Nadia Romiti ◽  
Federica Pellati ◽  
Paola Nieri ◽  
Stefania Benvenuti ◽  
Barbara Adinolfi ◽  
...  
Keyword(s):  
Cell Line ◽  
Inhibitory Activity ◽  
Proximal Tubular Cell ◽  
Tubular Cell ◽  
P Glycoprotein ◽  
Echinacea Pallida ◽  
Proximal Tubular

The Inhibitory Activity of Plants from Central Argentina on p-Hydroxyphenylpyruvate Dioxygenase. Isolation and Mechanism of Inhibition of a Flavanone from Flourensia oolepis

Planta Medica ◽  
2015 ◽  
Vol 81 (15) ◽  
pp. 1382-1391 ◽  
Author(s):  
María Chiari ◽  
Leonardo Tosoni ◽  
Mariana Joray ◽  
Georgina Diaz Napal ◽  
Sara Palacios ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Central Argentina ◽  
Mechanism Of Inhibition

scholarly journals From Taxuspine X to Structurally Simplified Taxanes with Remarkable P-Glycoprotein Inhibitory Activity

2010 ◽  
Vol 1 (8) ◽  
pp. 416-421 ◽  
Author(s):  
Daniele Castagnolo ◽  
Lorenzo Contemori ◽  
Giorgio Maccari ◽  
Stanislava I. Avramova ◽  
Annalisa Neri ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
P Glycoprotein
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